GSK2807 Trifluoroacetate

GSK2807 Trifluoroacetate is a selective and SAM-competitive inhibitor of SMYD3 (Ki: 14 nM; IC50: 130 nM) .GSK2807, a potent and selective, SAM-competitive inhibitor of SMYD3 (Ki = 14 nM) . A high-resolution crystal structure reveals that GSK2807 bridges the gap between the SAM-binding pocket and the substrate lysine tunnel of SMYD3. GSK2807 is 24-fold selective for SMYD3 in comparison with the closely related enzyme SMYD2 (Ki=14±6 nM and 345±36 nM, respectively) .